Design, synthesis and biological evaluation of heterocyclic azoles derivatives containing pyrazine moiety as potential telomerase inhibitors

YB Zhang, XL Wang, W Liu, YS Yang, JF Tang…

文献索引：Zhang, Yan-Bin; Wang, Xiao-Liang; Liu, Wen; Yang, Yu-Shun; Tang, Jian-Feng; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 21 p. 6356 - 6365

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被引用次数: 13

摘要

Three series of novel heterocyclic azoles derivatives containing pyrazine (5a–5k, 8a–8k and 11a–11k) have been designed, synthesized, structurally determined, and their biological activities were evaluated as potential telomerase inhibitors. Among the oxadiazole derivatives, compound 5c showed the most potent biological activity against SW1116 cancer cell line (IC50= 2.46 μM against SW1116 and IC50= 3.55 μM for telomerase). Compound ...